Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof,
wherein X
1
, X
2
, X
3
, X
4
, J, K, L, X
5
, X
6
, R
b
, G
2
, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
3,4-Disubstituted piperidines were synthesized through anti SN2′ allylation of 4-substituted 2-cyclopentenyl esters with reagents based on RMgX and CuX, thus allowing equal access to both trans- and cis-isomers. As an application, the paroxetine intermediate was synthesized efficiently. During the investigation, the MeOCH2CO2 group was found to show high reactivity in the pivotal anti SN2′ type reaction
3,4-二取代的哌啶是通过抗小号合成Ñ 2'的具有基于RMGX和的CuX试剂4-取代的2-环戊烯基酯烯丙基化,从而允许两者相等访问反式-和顺式-异构体。作为一种应用,高效合成了帕罗西汀中间体。在研究过程中,发现使用(i -PrO)Me 2 SiCH 2 MgCl和CuCN衍生的试剂,MeOCH 2 CO 2基团在关键的反S N 2'型反应中显示出高反应活性。
TRPV1 antagonists
申请人:Gomtsyan Arthur
公开号:US08802711B2
公开(公告)日:2014-08-12
Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates, or combinations thereof,
wherein X1, X2, X3, X4, J, K, L, X5, X6, Rb, G2, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
Rhodium-Catalyzed Asymmetric Allylic Substitution with Boronic Acid Nucleophiles
作者:Frederic Menard、Timothy M. Chapman、Chris Dockendorff、Mark Lautens
DOI:10.1021/ol061777l
日期:2006.9.1
An enantio-, regio-, and diastereoselective rhodium(I)-catalyzed desymmetrization of a meso-cyclic allylic dicarbonate with organoboronic acid nucleophiles is described. The rhodium(I) catalyst formed in situ from [Rh(cod)OH](2) and Xyl-P-PHOS allowed the S(N)2' allylic substitution product to be obtained with a range of arylboronic acids in enantiomeric excesses of up to 92% with regioselectivities of up to > 20:1.
TUETING, DAVID R.;ECHAVARREN, ANTONIO M.;STILLE, J. K., TETRAHEDRON, 45,(1989) N, C. 979-992
作者:TUETING, DAVID R.、ECHAVARREN, ANTONIO M.、STILLE, J. K.